During the past decade, the relationship between monoamine uptake and a variety of diseases and conditions has been appreciated and investigated. For example, the hydrochloride salt of fluoxetine (d1- N-methyl-3-[4-(trifluoromethyl)phenoxy]-3-phenylpropylamine) is a selective serotonin (5-hydroxytryptamine, 5HT) uptake inhibitor. Fluoxetine hydrochloride is marketed under the trademark PROZAC.RTM. for the treatment of depression. This compound is among many taught in U.S. Pat. No. 4,018,895, 4,194,009, and 4,314,081 as being potent, selective blockers of serotonin uptake.
Fluoxetine is a racemate of the two enantiomeric forms. The biological and pharmacological activity of each enantiomer has been reported to be essentially the same; see, Robertson et al., J. Med. Chem., 31, 1412 (1988) and references cited therein.
we have now discovered that the (R)-enantiomer of fluoxetine is a selective agonist of 5HT.sub.1C receptors.